Ceftaroline

Ceftaroline fosamil is an intravenous fifth-generation cephalosporin antibiotic. It is administered as a prodrug that is rapidly converted to the active agent ceftaroline, and it is sold under the brand name Teflaro among others. It was approved for clinical use in the United States in 2010 for acute bacterial skin and skin structure infections and later for community-acquired bacterial pneumonia.

Ceftaroline exerts its antibacterial effect by binding to penicillin-binding proteins, thereby inhibiting cell wall synthesis. Its most notable feature among cephalosporins is its activity against methicillin-resistant Staphylococcus aureus (MRSA) due to high affinity for PBP2a. The spectrum includes many Gram-positive cocci, particularly MRSA and penicillin-susceptible streptococci, with activity against Streptococcus pneumoniae as well. Activity against Enterococcus species is limited, and the agent generally has little or no activity against Pseudomonas aeruginosa. Its Gram-negative activity is variable and generally more limited than in earlier cephalosporins.

In clinical practice, ceftaroline is indicated for acute bacterial skin and skin structure infections and for community-acquired bacterial pneumonia. The usual adult dose is 600 mg given by intravenous infusion every 12 hours, with adjustments possible for renal impairment. It is administered as an IV infusion over a period of time appropriate to the formulation.

Common adverse effects include diarrhea, nausea, rash, and headache. Allergic reactions and Clostridioides difficile infection are potential risks, as with other beta-lactams. Resistance can arise from reduced affinity for the target PBPs or other beta-lactamase–mediated mechanisms.